(2R)-1-苄基-N-(3-螺[异苯并呋喃-1(3H),4'-哌啶]-1'-丙基)-2-吡咯烷甲酰胺

• 常用名: (2R)-1-苄基-N-(3-螺[异苯并呋喃-1(3H),4'-哌啶]-1'-丙基)-2-吡咯烷甲酰胺
• 英文名: BAN ORL 24
• CAS号: 475150-69-7
• 分子量: 433.59
• 密度: N/A
• 沸点: N/A
• 分子式: C₂₇H₃₅N₃O₂
• 熔点: N/A
• 闪点: N/A

用途

BAN ORL24游离碱是一种伤害肽/孤啡肽FQ(N/OFQ)肽受体(NOP)拮抗剂。BAN ORL24自由基对CHO细胞伤害肽(NOP)受体具有拮抗作用,KI值为0.24nM。BAN ORL 24游离碱可用于癌症和镇痛药的研究[1]。

名称

• 中文名: (2R)-1-苄基-N-(3-螺[异苯并呋喃-1(3H),4'-哌啶]-1'-丙基)-2-吡咯烷甲酰胺
• 英文名: 1-Benzyl-N-[3-(1'H,3H-spiro[2-benzofuran-1,4'-piperidin]-1'-yl)propyl]-D-prolinamide dihydrochloride

生物活性

• 描述: BAN ORL24游离碱是一种伤害肽/孤啡肽FQ(N/OFQ)肽受体(NOP)拮抗剂。BAN ORL24自由基对CHO细胞伤害肽(NOP)受体具有拮抗作用,KI值为0.24nM。BAN ORL 24游离碱可用于癌症和镇痛药的研究[1]。
• 相关类别:
  研究领域 >> 癌症
  信号通路 >> G 蛋白偶联受体/G 蛋白 >> 阿片受体
  信号通路 >> 神经信号通路 >> 阿片受体
• 体外研究: 禁令ORL 24是 NOR和 MOR(阿片受体亚型)拮抗剂,IC50值分别为 50微米和 0.224μM[2]
• 体内研究: BAN ORL 24(10 mg/kg静脉注射)会减弱 BPRIM97热镇痛作用的持续时间[3]
• 参考文献:

  [1]. Tao Hou, et al. Label-free cell phenotypic study of opioid receptors and discovery of novel mu opioid ligands from natural products. J Ethnopharmacol

  [2]. Chao, et al. BPR1M97, a dual mu opioid receptor/nociceptin-orphanin FQ peptide receptor agonist, produces potent antinociceptive effects with safer properties than morphine. Neuropharmacology 166, 107678 (2020).

  [3]. Fischetti et al (2009) Pharmacological characterization of the nociceptin/orphanin FQ receptor non peptide antagonist compound 24. Eur.J.Pharmacol. 614 50.

物理化学性质

• 分子式: C₂₇H₃₅N₃O₂
• 分子量: 433.59
• 精确质量: 505.226288
• InChIKey: MAKMQGKJURAJEN-RUZDIDTESA-N
• SMILES: O=C(NCCCN1CCC2(CC1)OCc1ccccc12)C1CCCN1Cc1ccccc1

靶点实验

查看更多实验

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实验名称：Effect on N/OFQ-induced pronociciceptive activity in Swiss albino mouse at 10 mg/kg, ... 来源：ChEMBL 靶标：Mus musculus External Id：CHEMBL1785660

实验名称：Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells 来源：ChEMBL 靶标：Nociceptin receptor External Id：CHEMBL867087

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实验名称：Antagonist activity as % reversal against the reduction in locomotor activity produce... 来源：ChEMBL 靶标：Mus musculus External Id：CHEMBL865856

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英文别名

• 2-Pyrrolidinecarboxamide, 1-(phenylmethyl)-N-(3-spiro[isobenzofuran-1(3H),4'-piperidin]-1'-ylpropyl)-, (2R)-, hydrochloride (1:2)
• 1-Benzyl-N-[3-(1'H,3H-spiro[2-benzofuran-1,4'-piperidin]-1'-yl)propyl]-D-prolinamide dihydrochloride
• BAN ORL 24